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Cat. No.: HY-175837

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EGFR-IN-172

EGFR-IN-172 is a EGFR inhibitor. EGFR-IN-172 effectively inhibits the proliferation of non-small cell lung cancer (NSCLC) cells carrying the L858R, T790M and C797S drug-resistant mutations. EGFR-IN-172 inhibits EGFR phosphorylation, induces cell cycle arrest and apoptosis. EGFR-IN-172 can be used for the study of NSCLC.

For research use only. We do not sell to patients.

CAS No.: 878416-74-1
Formula: C₂₂H₁₈FN₃O
Molecular Weight:359.40

Storage:

Please store the product under the recommended conditions in the Certificate of Analysis.

Data Sheet (273 KB)

EGFR-IN-172 Chemical Structure

CAS No.: 878416-74-1

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Antibody-Drug Conjugates

One-stop solution for XDC (ADC/PDC/RDC/ApDC/FDC/ISAC/VDC/SMDC)

Biological Activity
- Description
- Cellular Effect
- In Vitro
Chemical Information
Purity & Documentation
References
Calculators
Help & FAQs
Classifications
Bioz

Biological Activity

Description

All EGFR Isoforms :

Cellular Effect

Cell Line	Type	Value	Description	References
U-87MG ATCC	IC₅₀	9.2 μM Compound: CD373	Cytotoxicity against human U-87 MG cells assessed as growth inhibition measured after 72 hrs by MTT assay Cytotoxicity against human U-87 MG cells assessed as growth inhibition measured after 72 hrs by MTT assay	[PMID: 32830969]

In Vitro

EGFR-IN-172 (Compound 2b) shows high antiproliferative activity against A549 cells (EGFR^WT) (IC₅₀ = 5.31 μM), PC-9 cell (EGFR^T790M) (IC₅₀ = 0.55 μM), H1975 cells (EGFR^L858R/T790M) (IC₅₀ = 0.40 μM) and Ba/F3-EGFR^{L858R/T790M/C797S} cells (IC₅₀ = 2.36 μM)^[1].
EGFR-IN-172 (0.1-10 μM) inhibits the phosphorylation of EGFR (pEGFR) in H1975 and Ba/F3 triple-mutant cells in a concentration-dependent manner^[1].
EGFR-IN-172 (0.25-1 μM, 48 h) arrests the H1975 cells in the G0/G1 phase, but has no significant effect on the cell cycle of the Ba/F3 triple-mutant cells^[1].
EGFR-IN-172 (0.25-1 μM, 48 h) induces apoptosis in H1975 and Ba/F3 triple-mutant cells in a concentration-dependent manner^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Cycle Analysis^[1]

Cell Line:

H1975 and Ba/F3-EGFR^{L858R/T790M/C797S} cells
Concentration:

0.25, 0.5 and 1 μM
Incubation Time:

48 h
Result:

Arrested H1975 cells in the G0/G1 phase of the cell cycle.
Did not affect Ba/F3-EGFR^{L858R/T790M/C797S} cells.

Apoptosis Analysis^[1]

Cell Line:

H1975 and Ba/F3-EGFR^{L858R/T790M/C797S} cells
Concentration:

0.25, 0.5 and 1 μM
Incubation Time:

48 h
Result:

Effectively induced apoptosis in two EGFR mutant lung cancer cells.

Western Blot Analysis^[1]

Cell Line:

H1975 and Ba/F3-EGFR^{L858R/T790M/C797S} cells
Concentration:

0.25, 0.5 and 1 μM
Incubation Time:

48 h
Result:

Inhibited the phosphorylation of EGFR in a concentration-dependent manner in both cell lines.

Chemical Information

CAS No. 878416-74-1
Molecular Weight 359.40
Formula C₂₂H₁₈FN₃O
SMILES

OC1=C2N=CC=CC2=CC=C1C(C3=CC=CC(F)=C3)NC4=NC=CC(C)=C4
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (273 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

References

[1]. Xu X, et al. Design and synthesis of Betti base derivatives as EGFR inhibitors. Bioorg Chem. 2025 Sep;164:108872. [Content Brief]

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Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

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100 mg

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Biological Activity
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- In Vitro
Chemical Information
Purity & Documentation
References

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EGFR-IN-172

All EGFR Isoforms

Biological Activity

Chemical Information

Purity & Documentation

References

Calculators

Help & FAQs

EGFR-IN-172 Related Classifications

HY-175837 Related Classifications